This invention generally pertains to heterocyclic carbon compounds having drug and bio-affecting properties and to their preparation and use. In particular, the invention is concerned with 1,4-disubstituted piperazine derivatives wherein one substituent is 1,2-benzoisothiazol-3-yl or 1,2-benzisoxazol-2-yl and the other is a heterocycle (attached via an alkylene chain) or a butyrophenone-like (and corresponding carbinol) radical as depicted: ##STR1##
Wu, U.S. Pat. No. 3,398,151, Wu, et al., U.S. Pat. No. 3,717,634 and, respectively, corresponding Wu, et al., publications--J. Med. Chem., 12, 876-881 (1969), 15, 447-479 (1972)--variously describe azaspiro[4.5]decanedione and dialkylglutarimide psychotropic compounds resembling formula (1) ##STR2## wherein R.sup.1 and R.sup.2 are alkyl or joined to form --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 -- and B inter alia represents phenyl plus various heterocyclies (all with optional substituents): ##STR3##
Casten, et al., U.S. Pat. No. 4,182,763 concerns the anxiolytic use of compound (4) which is referred to in the biological literature as buspirone. ##STR4##
Benica, et al., J. Am. Pharmaceutical Association, 451-456 (1950) describes 3,3-dialkylglutarimides wherein R.sup.1 is C.sub.1-4 alkyl and R.sup.2 is hydrogen or C.sub.1-4 alkyl as shown in formula (3) and states the compounds lacked significant physiological activity. ##STR5##
Thiazolidinediones are known to the art. For example, Jones, et al., J. Chem. Soc., London, 91-92 (1946) refer to 5,5-dialkyl-2,4-thiazolidinedione barbituric acid analogs and disclose that a 5-spirocyclohexyl-2,4-thiazolidinedione (4) produced narcosis and analgesia in mice. ##STR6##
Various types of 1,4-substituted piperazine derivatives are also known to the art as illustrated in the following references.
Great Britain No. 2,023,594A discloses 1-(R-alkyl)-4-(3-trifluoromethylthiophenyl)piperazines useful for treating anxiety and depression having general formula (5) ##STR7## wherein n is 1-3 and R inter alia represents heterocycles such as ##STR8## wherein m is 0 or 1 and X is a --S--, --O--, imino, alkyl-imino or methylene.
Rojsner, et al., Collect. Czech. Chem. Commun., 40(4) 1218-1230 (1975) inter alia describe butyrophenone derivatives of formula (6) as part of a psychotropic structure-activity-relationship study. ##STR9##
None of the aforementioned references disclose or suggest the 1,2-benzisothiazole or 1,2-benzisoxazole piperazine derivatives of the instant invention.